203314-51-6Relevant articles and documents
Hepatitis C virus inhibitor and application thereof
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Paragraph 0239-0244, (2018/01/13)
The invention relates to a hepatitis C virus inhibitor and application thereof, and particularly discloses a compound which can be used as a hepatitis C virus and is as shown in a formula (I), or optical isomer, pharmaceutically acceptable salt, hydrate or solvate thereof, which can be used for treating hepatitis C virus (HCV) infection or hepatitis C diseases, or used as a hepatitis C virus nonstructural 5A (NS5A) protein inhibitor.
PROCESS FOR PREPARING TETRACYCLIC HETEROCYCLE COMPOUNDS
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Page/Page column 28; 29, (2015/05/19)
The present invention is directed to a process for preparing Tetracyclic Heterocycle Compounds of formula (I): which are useful as HCV NS5A inhibitors. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).
Enantioselective synthesis of an HCV NS5a antagonist
Mangion, Ian K.,Chen, Cheng-Yi,Li, Hongmei,Maligres, Peter,Chen, Yonggang,Christensen, Melodie,Cohen, Ryan,Jeon, Ingyu,Klapars, Artis,Krska, Shane,Nguyen, Hoa,Reamer, Robert A.,Sherry, Benjamin D.,Zavialov, Ilia
supporting information, p. 2310 - 2313 (2014/05/20)
A concise, enantioselective synthesis of the HCV NS5a inhibitor MK-8742 (1) is reported. The features of the synthesis include a highly enantioselective transfer hydrogenation of an NH imine and a dynamic diastereoselective transformation. The synthesis of this complex target requires simple starting materials and nine linear steps for completion.
Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity
Szczepankiewicz, Bruce G.,Kosogof, Christi,Nelson, Lissa T. J.,Liu, Gang,Liu, Bo,Zhao, Hongyu,Serby, Michael D.,Xin, Zhili,Liu, Mei,Gum, Rebecca J.,Haasch, Deanna L.,Wang, Sanyi,Clampit, Jill E.,Johnson, Eric F.,Lubben, Thomas H.,Stashko, Michael A.,Olejniczak, Edward T.,Sun, Chaohong,Dorwin, Sarah A.,Haskins, Kristi,Abad-Zapatero, Cele,Fry, Elizabeth H.,Hutchins, Charles W.,Sham, Hing L.,Rondinone, Cristina M.,Trevillyan, James M.
, p. 3563 - 3580 (2007/10/03)
The c-Jun N-terminal kinases (JNK-1, -2, and -3) are members of the mitogen activated protein (MAP) kinase family of enzymes. They are activated in response to certain cytokines, as well as by cellular stresses including chemotoxins, peroxides, and irradiation. They have been implicated in the pathology of a variety of different diseases with an inflammatory component including asthma, stroke, Alzheimer's disease, and type 2 diabetes mellitus. In this work, high-throughput screening identified a JNK inhibitor with an excellent kinase selectivity profile. Using X-ray crystallography and biochemical screening to guide our lead optimization, we prepared compounds with inhibitory potencies in the low-double-digit nanomolar range, activity in whole cells, and pharmacokinetics suitable for in vivo use. The new compounds were over 1000-fold selective for JNK-1 and -2 over other MAP kinases including ERK2, p38α, and p38δ and showed little inhibitory activity against a panel of 74 kinases.